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    • 4. 发明授权
    • Imidazole derivatives
    • 咪唑衍生物
    • US06288061B1
    • 2001-09-11
    • US09598216
    • 2000-06-21
    • Hiroyuki SueokaJouji YasuokaAkira NishiyamaMasatoshi KiuchiKatsuya YamamotoKunio SugaharaSyuji EharaKei Sakata
    • Hiroyuki SueokaJouji YasuokaAkira NishiyamaMasatoshi KiuchiKatsuya YamamotoKunio SugaharaSyuji EharaKei Sakata
    • A61K314178
    • C07D401/04C07D233/66C07D403/12C07D417/12C07D417/14
    • The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof. The compounds of the formulas (I) and (XII) and pharmaceutically acceptable salts thereof of the present invention inhibit IL-4 and IL-5 production by Th2 cells and are effective for the prophylaxis and treatment of allergic diseases such as atopic dermatitis, bronchial asthma, allergic rhinitis and the like.
    • 本发明涉及下式(I)的咪唑衍生物,其中R 1是氢,任选取代的烷基等,R 2是氢,任选取代的烷基等,R 3是任选取代的杂芳基,R 4是任选取代的环烷基,任选地 取代的苯基等,条件是当R 1为氢时,R 2和R 4相同或不同,并且各自为苯基或被卤素原子取代的苯基,低级烷基或低级烷氧基,R 3为被苯基取代的苯并噻唑基或噻唑基,咪唑 下式(Ⅻ)的衍生物,其中R 6是任选取代的苯基或任选取代的杂芳基且R 7是取代的苯基,及其药学上可接受的盐。 本发明的式(I)和(XII)化合物及其药学上可接受的盐抑制Th2细胞的IL-4和IL-5产生,对预防和治疗变应性疾病如特应性皮炎,支气管 哮喘,过敏性鼻炎等。
    • 7. 发明申请
    • 2-Aminobutanol Compound and Use Thereof for Medical Purposes
    • 2-氨基丁醇化合物及其用途
    • US20090082311A1
    • 2009-03-26
    • US12226745
    • 2007-04-27
    • Masatoshi KiuchiMitsuharu NakamuraMaiko HamadaKunio Sugahara
    • Masatoshi KiuchiMitsuharu NakamuraMaiko HamadaKunio Sugahara
    • A61K31/137C07C215/20C07C69/34C07D317/30A61P37/00A61K31/675A61K31/662A61K31/216C07F9/653A61K31/357
    • C07F9/653C07C217/64C07C225/16C07C309/65C07C323/32C07C323/38C07C323/41C07D333/22C07D333/34C07F9/091
    • The present invention provides a novel compound having few side effects such as bradycardia and the like and having superior peripheral blood lymphocyte-decreasing effect.The present invention provides a 2-aminobutanol compound represented by the following formula (I) wherein R1 is a hydrogen atom or P(═O) (OH)2, R2 is an alkyl having 1 to 4 carbon atoms optionally substituted by hydroxyl group(s) or optionally substituted by halogen atom(s), R3 is a hydrogen atom; a halogen atom; cyano; an alkyl having 1 to 4 carbon atoms optionally substituted by halogen atom(s); or an acyl having 2 to 5 carbon atoms optionally substituted by halogen atom(s), X is an oxygen atom, a sulfur atom, carbonyl or NR4 wherein R4 is a hydrogen atom or an alkyl having 1 to 4 carbon atoms, Ar1 is an optionally substituted arylene or an optionally substituted heteroarylene, and Ar2 is an optionally substituted aryl or an optionally substituted heteroaryl, provided that when X is an oxygen atom, Ar1 is phenylene and Ar2 is phenyl, then the phenyl for Ar2 should be substituted, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof, as well as a production method of the above-mentioned 2-aminobutanol compound.
    • 本发明提供一种副作用少的新型化合物,如心动过缓等,具有优异的外周血淋巴细胞减少作用。 本发明提供由下式(I)表示的2-氨基丁醇化合物,其中R 1为氢原子或P(-O)(OH)2,R 2为任选被羟基取代的具有1至4个碳原子的烷基 或任选被卤素原子取代,R 3是氢原子; 卤素原子; 氰基; 任选被卤素原子取代的碳原子数1〜4的烷基; 或任选被卤素原子取代的具有2至5个碳原子的酰基,X是氧原子,硫原子,羰基或NR 4,其中R 4是氢原子或具有1至4个碳原子的烷基,Ar 1是 任选取代的亚芳基或任选取代的亚杂芳基,Ar 2是任选取代的芳基或任选取代的杂芳基,条件是当X是氧原子时,Ar 1是亚苯基,Ar 2是苯基,则Ar 2的苯基应该被取代,或 其药学上可接受的酸加成盐或其水合物或其溶剂合物,以及上述2-氨基丁醇化合物的制备方法。
    • 8. 发明授权
    • Benzene compound and pharmaceutical use thereof
    • 苯化合物及其药物用途
    • US06187821B1
    • 2001-02-13
    • US09309818
    • 1999-05-12
    • Tetsuro FujitaKunitomo AdachiToshiyuki KoharaMasatoshi KiuchiKenji ChibaKoji TeshimaTadashi Mishina
    • Tetsuro FujitaKunitomo AdachiToshiyuki KoharaMasatoshi KiuchiKenji ChibaKoji TeshimaTadashi Mishina
    • A61K31135
    • C07C215/56C07C215/28C07C215/30C07C217/64C07C217/72C07C219/22C07C225/16C07C233/18C07C233/31C07C233/36C07C233/73C07C271/16C07C271/18C07C2601/02
    • A benzene compound of the formula: wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behcet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary, cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective-tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma and pollinosis. It is useful also as an antifungal agent and hair growth stimulant.
    • 一种下式的苯化合物:其中每个符号如说明书中所定义;光学活性异构体或其盐,含有该化合物的药用组合物和含有该有效成分的免疫抑制剂。化合物,旋光异构体或 盐具有优异的免疫抑制作用,可用作器官或骨髓移植中发生的排斥反应的抑制剂,并且作为关节风湿病,特应性湿疹(皮炎),贝切特氏病,葡萄膜疾病,系统性红斑狼疮, Sjögren综合征,多发性硬化症,重症肌无力,I型糖尿病,内分泌眼病,原发性胆汁性肝硬化,克罗恩病,肾小球性肾炎,结节病,牛皮癣,天疱疮,再生障碍性贫血,特发性血小板减少性紫癜,变态反应,结节性多动脉炎,进行性系统性硬化症 组织病,主动脉炎综合征,多发性肌炎,皮肌炎,威基 r肉芽肿,溃疡性结肠炎,活动性慢性肝炎,自身免疫性溶血性贫血,伊文思综合征,支气管哮喘和花粉症。 它也可用作抗真菌剂和毛发生长兴奋剂。
    • 10. 发明授权
    • Benzene compound and pharmaceutical use thereof
    • 苯化合物及其药物用途
    • US06372800B1
    • 2002-04-16
    • US09691099
    • 2000-10-19
    • Tetsuro FujitaKunitomo AdachiToshiyuki KoharaMasatoshi KiuchiKenji ChibaKoji TeshimaTadashi Mishina
    • Tetsuro FujitaKunitomo AdachiToshiyuki KoharaMasatoshi KiuchiKenji ChibaKoji TeshimaTadashi Mishina
    • A61K3135
    • C07C215/56C07C215/28C07C215/30C07C217/64C07C217/72C07C219/22C07C225/16C07C233/18C07C233/31C07C233/36C07C233/73C07C271/16C07C271/18C07C2601/02
    • A benzene compound of the formula wherein each symbol is as defined in the specification; an optically active isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, optically active isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation, and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behcet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary, cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective-tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma and pollinosis. It is useful also as an antifingal agent and hair growth stimulant.
    • 每个符号的苯甲醛的苯化合物如说明书中所定义; 其光学活性异构体或其盐,含有它们的药用组合物和含有该活性成分的免疫抑制剂。该化合物,旋光异构体或盐具有优异的免疫抑制作用,可用作抑制反应发生的抑制剂 在器官或骨髓移植中,作为关节风湿病,特应性湿疹(皮炎),贝切特氏病,葡萄膜疾病,系统性红斑狼疮,Sjögren综合征,多发性硬化症,重症肌无力,I型糖尿病,内分泌眼病,原发性 胆汁,肝硬化,克罗恩病,肾小球肾炎,结节病,牛皮癣,天疱疮,再生障碍性贫血,特发性血小板减少性紫癜,变态反应,结节性多动脉炎,进行性系统性硬化症,混合性结缔组织病,主动脉炎综合征,多发性肌炎,皮肌炎,韦格纳肉芽肿,溃疡性结肠炎, 活动性慢性肝炎,自身免疫性溶血性贫血, 伊文思综合征,支气管哮喘和花粉症。 它也可用作抗衰老剂和毛发生长兴奋剂。